초록 ▼

The present invention involves a process for producing fine powder suitable for the preparation of antifungal polyene microlide-containing liposomes upon suspension in an aqueous solution. This process comprises the following steps. Quantities of polyene macrolide and phospholipids are dissolved res

The present invention involves a process for producing fine powder suitable for the preparation of antifungal polyene microlide-containing liposomes upon suspension in an aqueous solution. This process comprises the following steps. Quantities of polyene macrolide and phospholipids are dissolved respectively in a first solvent and a second solvent to form a first solution and a second solution. The first solution and the second solution are mixed in a desired ratio to form a mixture. The first solvent and the second solvent are then removed from the mixture, for example by evaporation, to form a residue. The residue is then dissolved in a third solvent comprising tertiary butanol and methylene chloride to form a third solution. The third solvent is then removed from the third solution to form a remnant. The remnant is then dissolved in a solvent consisting essentially of tertiary butanol to form a fourth solution. The fourth solution is then filtered through a filter having orifices of between about 0.05 and 0.5 micrometers in diameter to produce a filtrate. The filtrate is lyophilized to remove the tertiary butanol and a fine powder remains. This fine powder may be used to form polyene macrolide-containing liposomes by simple incubation or suspension in an aqueous solution.

대표청구항 ▼

A process for producing a powder which forms liposomes comprising an antifungal polyene macrolide upon suspension in an aqueous solution, said process comprising the steps of: (a) dissolving antifungal polyene macrolide and phospholipids in a quantity of first organic solvent and a quantity of secon

A process for producing a powder which forms liposomes comprising an antifungal polyene macrolide upon suspension in an aqueous solution, said process comprising the steps of: (a) dissolving antifungal polyene macrolide and phospholipids in a quantity of first organic solvent and a quantity of second organic solvent respectively, to form a first solution and a second solution; (b) mixing the first solution and the second solution to form a mixture; (c) removing the first organic solvent and the second organic solvent from the mixture to form a residue; (d) dissolving the residue in a quantity of a third organic solvent to form a third solution, wherein the third organic solvent comprises tertiary butanol and methylene chloride; (e) extracting the third organic solvent from the third solution to leave a remnant; (f) forming a fourth solution by dissolving the remnant in a solvent consisting essentially of tertiary butanol; (g) passing the fourth solution through a filter having orifices with diameters of between about 0.05 um and about 0.5 um to produce a filtrate; and (h) lyophilizing the filtrate to remove the solvent consisting essentially of tertiary butanol. The process of claim 1 wherein the antifungal polyene macrolide is nystatin, amphotericin B, partricin or a derivative thereof.